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Review ArticleReview Article

Mu Opioids and Their Receptors: Evolution of a Concept

Gavril W. Pasternak and Ying-Xian Pan
David R. Sibley, ASSOCIATE EDITOR
Pharmacological Reviews October 2013, 65 (4) 1257-1317; DOI: https://doi.org/10.1124/pr.112.007138
Gavril W. Pasternak
Molecular Pharmacology and Chemistry Program and Department of Neurology, Memorial Sloan-Kettering Cancer Center, New York, New York
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Ying-Xian Pan
Molecular Pharmacology and Chemistry Program and Department of Neurology, Memorial Sloan-Kettering Cancer Center, New York, New York
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David R. Sibley
Molecular Pharmacology and Chemistry Program and Department of Neurology, Memorial Sloan-Kettering Cancer Center, New York, New York
Roles: ASSOCIATE EDITOR
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Abstract

Opiates are among the oldest medications available to manage a number of medical problems. Although pain is the current focus, early use initially focused upon the treatment of dysentery. Opium contains high concentrations of both morphine and codeine, along with thebaine, which is used in the synthesis of a number of semisynthetic opioid analgesics. Thus, it is not surprising that new agents were initially based upon the morphine scaffold. The concept of multiple opioid receptors was first suggested almost 50 years ago (Martin, 1967), opening the possibility of new classes of drugs, but the morphine-like agents have remained the mainstay in the medical management of pain. Termed mu, our understanding of these morphine-like agents and their receptors has undergone an evolution in thinking over the past 35 years. Early pharmacological studies identified three major classes of receptors, helped by the discovery of endogenous opioid peptides and receptor subtypes—primarily through the synthesis of novel agents. These chemical biologic approaches were then eclipsed by the molecular biology revolution, which now reveals a complexity of the morphine-like agents and their receptors that had not been previously appreciated.

Footnotes

  • This work was supported in part by the National Institutes of Health National Institute on Drug Abuse [Grants DA00220, DA02615, DA06241, DA07242] (to G.W.P.) and [Grants DA013997 and DA029244] (to X.Y.P.).

  • dx.doi.org/10.1124/pr.112.007138

  • Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics
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Pharmacological Reviews: 65 (4)
Pharmacological Reviews
Vol. 65, Issue 4
1 Oct 2013
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Review ArticleReview Article

Mu Opioids and Their Receptors: Evolution of a Concept

Gavril W. Pasternak and Ying-Xian Pan
Pharmacological Reviews October 1, 2013, 65 (4) 1257-1317; DOI: https://doi.org/10.1124/pr.112.007138

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Review ArticleReview Article

Mu Opioids and Their Receptors: Evolution of a Concept

Gavril W. Pasternak and Ying-Xian Pan
Pharmacological Reviews October 1, 2013, 65 (4) 1257-1317; DOI: https://doi.org/10.1124/pr.112.007138
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  • Article
    • Abstract
    • I. Historical Overview
    • II. Opioids
    • III. Mu Opiate Pharmacology
    • IV. Opioid Binding Sites: Early Studies
    • V. Pharmacological Evidence for Multiple Mu Receptor Subtypes
    • VI. Molecular Biology of Mu Receptors
    • VII. The OPRM1 Gene
    • VIII. Alternative Splicing of the OPRM1 Genes
    • IX. The Future
    • Acknowledgments
    • Authorship Contributions
    • Footnotes
    • Abbreviations
    • References
  • Figures & Data
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